Bepotastine|125602-71-3|(贝他斯汀)-陌孚医药/Medlife

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Bepotastine (Synonyms: 贝他斯汀)

目录号: PL14988 纯度: ≥98%

CAS No. :125602-71-3

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中文名称	Bepotastine
中文别名	贝托斯汀;4-[4-[(4-氯苯基)吡啶-2-基甲氧基]哌啶-1-基]丁酸;(+)-(S)-4-[4-[1-(4-氯苯基)-1-(2-吡啶)甲氧基]哌啶-1-基]丁酸;贝托斯汀杂质;贝托斯汀杂质标准品对照品;贝托司汀
英文名称	Bepotastine
英文别名	(S)-4-(4-((4-Chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid;4-[4-[(4-Chlorophenyl)pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid;4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-1-Piperidinebutanoic acid;BEPOTASTINE;(+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid monobenzenesulfonate;(+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]pip;(+)-(S)-4-{4[(4-chlorphenyl)(2-pyridil)methoxy]piperidino}butyric acid monobenzenesulfonate;1-Piperidinebutanoic acid,4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy];4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy];betotastine besilate;-4-(4-((4-Chlorophenyl);4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy]-;4-(4-[(1S)(4-CHLOROPHENYL)-2-PYRIDYLMETHOXY]PIPERIDYL)BUTANOIC ACID;1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-;(+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid;Bepotastine
Cas No.	125602-71-3
分子式	C₂₁H₂₅N₂O₃Cl
分子量	388.89
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Bepotastine 是一种具有选择性和口服活性的第二代组胺 H1 受体 (histamine H1 receptor) 拮抗剂，可抑制组胺介导的神经生长因子 (NGF) 表达上调。Bepotastine 可用于过敏性鼻炎，过敏性结膜炎和荨麻疹/瘙痒症的研究。

生物活性

Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.

性状

Liquid

IC50 & Target[1][2]

Histamine H1 Receptor

体外研究(In Vitro)

Bepotastine (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.
Bepotastine (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

体内研究(In Vivo)

Bepotastine (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration.
Bepotastine (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control.
Bepotastine (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Kida T, et al. Bepotastine besilate, a highly selective histamine H(1) receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp Eye Res. 2010 Jul;91(1):8
[2]. Kamata Y, et al. Bepotastine besilate downregulates the expression of nerve elongation factors in normal human epidermal keratinocytes. J Dermatol Sci. 2018 Apr 23:S0923-1811(18)30186-5.

溶解度数据	In Vitro: DMSO : 100 mg/mL (257.14 mM; Need ultrasonic)H₂O : ≥ 100 mg/mL (257.14 mM)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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